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1999 terpenes terpenes U 0200 17 - 183 Novel Cytokine Release Inhibitors. Part 3. Truncated Analogues of Tripterine. Various truncated analogues of tripterine such as (XII), (XIII) and (XIV) are synthesized using the tricyclic and the tetracyclic interme- diates (IX) and (VIII), resp., as the key substrates. It is clearly demonstrated that the small synthetic compounds have good cytokine release inhibitory effects, although less potent than tripterine. Moreover, it is established that the primary pharmacophore resides on the A/B rings. — (HE, WEI; HUANG, FU-CHIH; GAVAI, ASHVIN; CHAN, WAN K.; AMATO, GEORGE; YU, KIN-TAK; ZILBERSTEIN, ASHER; Bioorg. Med. Chem. Lett. 8 (1998) 24, 3659-3664; Dep. Med. Chem., Rhone-Poulenc Rorer Cent. Res., Collegeville, PA 19426, USA; EN) 1

ChemInform Abstract: Novel Cytokine Release Inhibitors. Part 3. Truncated Analogues of Tripterine

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Page 1: ChemInform Abstract: Novel Cytokine Release Inhibitors. Part 3. Truncated Analogues of Tripterine

1999 terpenes

terpenesU 0200

17 - 183Novel Cytokine Release Inhibitors. Part 3. Truncated Analogues ofTripterine. — Various truncated analogues of tripterine such as (XII),(XIII) and (XIV) are synthesized using the tricyclic and the tetracyclic interme-diates (IX) and (VIII), resp., as the key substrates. It is clearly demonstratedthat the small synthetic compounds have good cytokine release inhibitoryeffects, although less potent than tripterine. Moreover, it is established that theprimary pharmacophore resides on the A/B rings. — (HE, WEI; HUANG,FU-CHIH; GAVAI, ASHVIN; CHAN, WAN K.; AMATO, GEORGE; YU,KIN-TAK; ZILBERSTEIN, ASHER; Bioorg. Med. Chem. Lett. 8 (1998) 24,3659-3664; Dep. Med. Chem., Rhone-Poulenc Rorer Cent. Res., Collegeville,PA 19426, USA; EN)

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